Relaxant effects of quercetin methyl ether derivatives in isolated guinea pig trachea and their structure-activity relationships

Wun-Chang Ko, Shih W. Kuo, Joen Rong Sheu, Chien Huang Lin, Shu-Huey Tzeng, Chi Ming Chen

研究成果: 雜誌貢獻文章同行評審

16 引文 斯高帕斯(Scopus)

摘要

In the present study, we attempted to compare quercetin methyl ethers and to look for the structure-activity relationships, which may be helpful for synthesizing more active compounds for the treatment of asthma. Four present and two previously studied quercetin methyl ethers concentration- dependently relaxed histamine (30 μM), carbachol (0.2 μM) and KCl (30 mM) induced precontraction. According to their IC25 values to histamine- induced precontraction, the potency order was quercetin 3,3',4',5,7- pentamethyl ether (QPME), quercetin 3-methyl ether > quercetin, quercetin 3,4',7-trimethyl ether (ayanin) > quercetin 4'-methyl ether (tamarixetin), quercetin 3,3',4',7-tetramethyl ether (QTME). Therefore, the methylation at 3, at 5, and at both 3 and 7 positions of the A or/and C ring of quercetin nucleus may increase their tracheal relaxant activity. However, the methylation at the 3' and at the 4' position of the B ring of quercetin nucleus may decrease their tracheal relaxant activity.
原文英語
頁(從 - 到)273-275
頁數3
期刊Planta Medica
65
發行號3
出版狀態已發佈 - 1999

ASJC Scopus subject areas

  • 植物科學
  • 有機化學
  • 藥物發現
  • 藥理

指紋

深入研究「Relaxant effects of quercetin methyl ether derivatives in isolated guinea pig trachea and their structure-activity relationships」主題。共同形成了獨特的指紋。

引用此